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macitentan
EntityQ6724151· pop 12· linked from 159 articles

macitentan

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Also known as ACT-064992, ACT064992, ACT 064992

Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist developed by Actelion and approved for the treatment of pulmonary arterial hypertension (PAH). Macitentan is a dual endothelin receptor antagonist, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype.

Wikidata facts

Mass
585.9633483200003
Show 5 more facts
chemical formula
C₁₉H₂₀Br₂N₆O₄S
canonical SMILES
CCCNS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br
World Health Organisation international non-proprietary name
macitentan
defined daily dose
10
Commons category
Macitentan
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~4 min read

Article

7 sections
Contents
  • Adverse effects
  • Mechanism of action
  • Endothelin and endothelin receptors
  • Role of macitentan
  • Pharmacokinetics
  • Experimental pharmacokinetics
  • References

Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist developed by Actelion and approved for the treatment of pulmonary arterial hypertension (PAH). Macitentan is a dual endothelin receptor antagonist, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype.

Macitentan was approved for medical use in the United States in October 2013.

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